5-羟色胺（5-HT）和间氯苯哌嗪（m-CPP）对人体灌注血小板中[3H]-5-羟色胺流出的影响。
The effects of 5-HT and m-chlorophenylpiperazine (m-CPP) on the efflux of [3H]-5-HT from human perfused platelets.
作者信息
Carver J G, Grahame-Smith D G, Johnson E S, Madgwick Z
机构信息
MRC Unit, Radcliffe Infirmary.
出版信息
Br J Clin Pharmacol. 1993 May;35(5):473-8. doi: 10.1111/j.1365-2125.1993.tb04172.x.
Abstract
- m-Chlorophenylpiperazine (m-CPP), a 5-HT1c-receptor agonist, induces migraine-like headaches when taken orally by migraine sufferers. The present study was undertaken to see what effects m-CPP had on 5-HT function in platelets. 2. Platelets from healthy male volunteers were loaded with [3H]-5-HT and continuously perfused in vitro with carboxygenated Krebs solution at 37 degrees C. After 30 min washout the effects of m-CPP, thrombin, 5-HT and ADP on the efflux of [3H]-5-HT were recorded. 3. m-CPP (0.5-500 microM) did not evoke an increase in the efflux of [3H]-5-HT over that occurring spontaneously whereas thrombin, unlabelled 5-HT and ADP did. The effects of 5-HT were potentiated by ADP. The results were identical whether or not the 5-HT reuptake blocker paroxetine (1 microM) was present. 4. m-CPP inhibited the increase in the efflux of [3H]-5-HT evoked by different concentrations of unlabelled 5-HT in the presence of ADP (2.5 microM) and displaced the 5-HT log concentration response curve to the right. A similar result was obtained with the 5-HT2-receptor antagonist ketanserin. 5. We conclude that m-CPP is a 5-HT2-receptor antagonist on human platelets, which is unlikely to account for its headache-inducing property, as many drugs effective in migraine prophylaxis have this action.
摘要
- 间氯苯哌嗪（m-CPP）是一种5-HT1c受体激动剂，偏头痛患者口服后会诱发类似偏头痛的头痛。本研究旨在观察m-CPP对血小板中5-HT功能的影响。2. 从健康男性志愿者采集的血小板用[3H]-5-HT标记，于37℃在体外持续用充氧的 Krebs 溶液灌注。冲洗30分钟后，记录m-CPP、凝血酶、5-HT和ADP对[3H]-5-HT流出的影响。3. m-CPP（0.5 - 500微摩尔）不会引起[3H]-5-HT流出量比自发流出量增加，而凝血酶、未标记的5-HT和ADP会。5-HT的作用被ADP增强。无论是否存在5-HT再摄取阻滞剂帕罗西汀（1微摩尔），结果都是相同的。4. m-CPP在存在ADP（2.5微摩尔）的情况下，抑制不同浓度未标记5-HT引起的[3H]-5-HT流出量增加，并使5-HT对数浓度反应曲线右移。5-HT2受体拮抗剂酮色林也得到了类似结果。5. 我们得出结论，m-CPP是人类血小板上的5-HT2受体拮抗剂，这不大可能解释其诱发头痛的特性，因为许多对偏头痛预防有效的药物都有这种作用。
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引用本文的文献
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本文引用的文献
1
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Neuropharmacology. 1982 May;21(5):445-50. doi: 10.1016/0028-3908(82)90029-6.
2
Antagonism of vascular serotonin receptors by m-chlorophenylpiperazine and m-trifluoromethylphenylpiperazine.间氯苯哌嗪和间三氟甲基苯哌嗪对血管5-羟色胺受体的拮抗作用。
Life Sci. 1983 Feb 14;32(7):711-8. doi: 10.1016/0024-3205(83)90303-x.
3
Serotonin-releasing effects of substituted piperazines in vitro.取代哌嗪在体外的5-羟色胺释放效应
Biochem Pharmacol. 1984 May 1;33(9):1531-5. doi: 10.1016/0006-2952(84)90424-6.
4
Further evidence for negative feedback control of serotonin release in the central nervous system.中枢神经系统中血清素释放的负反馈控制的进一步证据。
Naunyn Schmiedebergs Arch Pharmacol. 1981 Aug;317(1):36-43. doi: 10.1007/BF00506254.
5
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J Pharm Pharmacol. 1981 Jul;33(7):477-8. doi: 10.1111/j.2042-7158.1981.tb13841.x.
6
Induction of migrainelike headaches by the serotonin agonist m-chlorophenylpiperazine.血清素激动剂间氯苯哌嗪诱发类偏头痛性头痛
Clin Pharmacol Ther. 1988 Jun;43(6):605-9. doi: 10.1038/clpt.1988.83.
7
Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors.哌嗪类药物在磷酸肌醇水解相关的5-羟色胺能（5-HT-2和5-HT-1c）受体上的相对效能
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